Wednesday, April 15, 2015

Hormone Therapy And Letrozole Benefits

Hormones are substances that function as chemical messengers in the body. They affect the actions of cells and tissues at various locations in the body, often reaching their targets through the bloodstream.

The hormones estrogen and progesterone are produced by the ovaries in premenopausal women and by some other tissues, including fat and skin, in both premenopausal and postmenopausal women. Estrogen promotes the development and maintenance of female sex characteristics and the growth of long bones. Progesterone plays a role in the menstrual cycle and pregnancy.

Estrogen and progesterone can also promote the growth of some breast cancers, which are called hormone-sensitive (or hormone-dependent) breast cancers. Hormone-sensitive breast cancer cells contain proteins known as hormone receptors that become activated when hormones bind to them. The activated receptors cause changes in the expression of specific genes, which can lead to the stimulation of cell growth.

To determine whether breast cancer cells contain hormone receptors, doctors test samples of tumor tissue that have been removed by surgery. If the tumor cells contain estrogen receptors, the cancer is called estrogen receptor-positive (ER-positive), estrogen-sensitive, or estrogen-responsive. Similarly, if the tumor cells contain progesterone receptors, the cancer is called progesterone receptor-positive (PR- or PgR-positive). Approximately 70 percent of breast cancers are ER-positive. Most ER-positive breast cancers are also PR-positive.

Breast cancers that lack estrogen receptors are called estrogen receptor-negative (ER-negative). These tumors are estrogen-insensitive, meaning that they do not use estrogen to grow. Breast tumors that lack progesterone receptors are called progesterone receptor-negative (PR- or PgR-negative).
Several strategies have been developed to treat hormone-sensitive breast cancer, including the following:

Blocking ovarian function: Because the ovaries are the main source of estrogen in premenopausal women, estrogen levels in these women can be reduced by eliminating or suppressing ovarian function. Blocking ovarian function is called ovarian ablation.

Ovarian ablation can be done surgically in an operation to remove the ovaries (called oophorectomy) or by treatment with radiation. This type of ovarian ablation is usually permanent.

Alternatively, ovarian function can be suppressed temporarily by treatment with drugs called gonadotropin-releasing hormone (GnRH) agonists, which are also known as luteinizing hormone-releasing hormone (LH-RH) agonists. These medicines interfere with signals from the pituitary gland that stimulate the ovaries to produce estrogen.

Blocking estrogen production: Drugs called aromatase inhibitors can be used to block the activity of an enzyme called aromatase, which the body uses to make estrogen in the ovaries and in other tissues. Aromatase inhibitors are used primarily in postmenopausal women because the ovaries in premenopausal women produce too much aromatase for the inhibitors to block effectively. However, these drugs can be used in premenopausal women if they are given together with a drug that suppresses ovarian function.

Examples of aromatase inhibitors approved by the FDA are anastrozole (Arimidex) and letrozole (Femara), both of which temporarily inactivate aromatase, and exemestane (Aromasin), which permanently inactivates the enzyme.

Blocking estrogen’s effects: Several types of drugs interfere with estrogen’s ability to stimulate the growth of breast cancer cells:

Selective estrogen receptor modulators (SERMs) bind to estrogen receptors, preventing estrogen from binding. Examples of SERMs approved by the FDA are tamoxifen (Nolvadex), raloxifene (Evista), and toremifene (Fareston). Tamoxifen has been used for more than 30 years to treat hormone receptor-positive breast cancer.

Because SERMs bind to estrogen receptors, they can potentially not only block estrogen activity (serve as estrogen antagonists) but also mimic estrogen effects (i.e., serve as estrogen agonists). Most SERMs behave as estrogen antagonists in some tissues and as estrogen agonists in other tissues. For example, tamoxifen blocks the effects of estrogen in breast tissue but acts like estrogen in the uterus and bone.
   
Other antiestrogen drugs, such as fulvestrant (Faslodex), work in a somewhat different way to block estrogen’s effects. Like SERMs, fulvestrant attaches to the estrogen receptor and functions as an estrogen antagonist. However, unlike SERMs, fulvestrant has no estrogen agonist effects. It is a pure antiestrogen. In addition, when fulvestrant binds to the estrogen receptor, the receptor is targeted for destruction.

An oral non-steroidal aromatase inhibitor, Letrozole is routinely prescribed by medical practitioners to patients with hormonally responsive breast cancer after surgery. Also known as Femara and Liquifem, the antiestrogen is also used by budding and professional sportsmen on anabolic steroids to keep off estrogenic side effects such as oily skin, acne, gynecomastia, and bloating at bay while reaping the optimum benefits of steroids during an anabolic steroid cycle.
Letrozole is considered as one of the most potent drugs for stimulating metabolic rate of the body and promoting burning of fat. It is also useful in reducing the levels of LDL (bad) cholesterol and promoting the level of spermatogenesis in male patients suffering from non-obstructive azoospermia and treat endometriosis. The third-generation selective oral aromatase inhibitor, Letrozole, is also used to stimulating dramatic enhancements in terms of growth hormone, cortisol, SHBG, hepatic production of binding proteins, HDL, and growth and development of sexual characteristics. If that was not all, Femara also has the ability to promote healthy immune function, healthy cholesterol levels, joint health, cognitive function, and muscle growth while reducing or even eliminating estrogenic side effects such as oily skin, gynecomastia, and fluid retention.

The medication may even be recommended by medical practitioners to treat certain types of breast cancer (such as hormone-receptor-positive breast cancer) in women after menopause or preventing the cancer from making a return. By reducing the amount of estrogens in the body, Letrozole helps in slowing or reversing the growth of these breast cancers.

The use of Letrozole, for a period of three to six weeks, is also associated with restoration of natural products of hormones, like testosterone. If that was not all, one 2.5 mg tablet of Femara is good enough to inhibit side effects of estrogens by as much as 80 percent.

The ideal dosage of Letrozole is 2.5 mg once a day for treating patients with breast cancer. Sportsmen use Letrozole in dosages of 0.5-1.0 mg every day, with or without meals. It is very important to note that this is a prescription drug and must be used and purchased only with a prescription. Moreover, its use should always be followed by a medical recommendation for the same after careful and complete evaluation of medical reports and history. At no point of time, two dosages of the drug can be taken together, even if missed accidentally. In case the first dose has been missed, it should be skipped and the next dose should be taken at its scheduled time.

Letrozole use is not recommended to pregnant and breastfeeding women and children or those having allergies to the drug or any of its ingredients. Those suffering with prostate, breast, or testicular cancer or treated for high blood pressure, liver damage, stroke, and kidney damage should avoid using the drug. Patients making use of drugs such as Prasterone, Tamoxifen, DHEA, and Androstenedione should avoid using Letrozole unless the same is specifically approved by a qualified medical practitioner.

The abuse of Letrozole can lead to side effects and thus best avoided. When abused or of a low grade, it can lead to side effects such as hot flushes, night sweats, vomiting, bone pain, loss of appetite, headache, stomach pain, cough, and breast pain. Use of Letrozole should not be made by individuals treated for high blood fats (cholesterol), bone problems (such as osteopenia, osteoporosis), stroke or blood clots, heart disease (such as chest pain, heart attack, heart failure), high blood pressure, kidney problems, and liver problems.

In rare cases, Femara use may cause severe health complications such as chest/jaw/left arm pain, confusion, coughing up blood, sudden dizziness/fainting, pain/swelling/warmth in the groin/calf, tingling/weakness/numbness in the arms/legs, weakness on one side of the body, vision changes, sudden/severe headache, slurred speech, bone fractures, mental/mood changes (such as depression, anxiety), swelling of arms/legs, and blurred vision. Drugs such as estrogens (such as ethinyl estradiol, conjugated estrogens), estrogen blockers (such as anastrozole, tamoxifen) may interfere with functioning and action mechanism of Letrozole and this may cause serious side effects or may cause the medications not to work correctly. The consumption of alcoholic beverages should be reduced, if the same cannot be completely eliminated, while Letrozole is being used.

Thursday, April 9, 2015

GP Proviron by Geneza Pharmaceuticals

Originally developed as a drug for treating depression in men, Proviron or Mesterolone is an orally applicable androgen and derivative of Dihydrotestosterone (DHT). Proviron is 1 alpha-methyl-17 beta-hydroxy-5 alpha-androstan-3-one and the molecular mass of this prescription drug is 304.467 g/mol at the base. One of the biggest advantages associated with use of GP Proviron is its unique ability to promote the count and quality of sperm and is also indicated to treat serious wellness problems such as low libido and erectile malfunction. The drug is even recommended to male patients struggling with impotency or lack of testosterone. In addition to these advantages, use of Mesterolone (GP Proviron) is also associated with improved release of luteinizing hormone and follicle-stimulating hormone for stimulating testes so that more testosterone can be produced.

Since it is not a 17 alpha alkylated compound, it can be used for a long period of time. The drug can even enhance potency of testosterone when used in an anabolic steroid cycle with it. The fact that GP Proviron can attach itself to SHBG (sex hormone-binding globulin) and albumin means that a large percentage of testosterone (free) is made available to conduct anabolic actions. Furthermore, the performance enhancing drug can also be used as an anti-aromatase and this characteristic proves to be beneficial when the drug is stacked with other anabolic steroids and performance enhancing drugs that may convert to estrogen to some extent. Since this steroid can bind to the aromatase enzyme, it does not allow steroids that are made a part of the cycle (with GP Proviron) to interact with enzymes and lead to formation of estrogens. Some sportsmen even use Mesterolone in an anabolic steroid cycle in place of testosterone that can have a negative effect on the libido since Proviron can enhance the level of libido to some extent because of the dihydrotestosterone effects of Mesterolone. A combined therapy with gonadotrophic hormone exhibiting follicle-stimulating hormone activity may be advised for initiating treatment and treatment with GP Proviron may be repeated after an interval of several weeks. It is important to note that use of Proviron is meant only for male patients though a medical practitioner may recommend its use to some female patients. When advised, individuals administered with it should undergo regular prostate examinations prophylactic-ally.

The increased level of free testosterone can then be utilized by the body for promoting protein synthesis that in turn stimulates muscle gain. Moreover, the steroid also has the ability to reduce the amount of free estrogen in the body by minimizing estrogen receptors’ ability to bind to estrogen. The drug is medically recommended to individuals suffering with potency disturbances due to androgen-deficiency, easy fatigability, lack of concentration, weak memory, disturbances of libido, depressive moods, general vegetative complaints, irritability, and declining physical activity and mental alertness in middle- and old-aged men. It may even be indicated for promoting the development of secondary male sex characteristics in cases of prepuberal hypogonadism and increasing fructose concentration up to normal values to enhance the chances of procreation.

The ideal dose of Mesterolone (GP Proviron) is 25-100 mg per day for men and 25 mg every day for women though some sportsmen, male as well as female, increase the doses to 50-125 mg every day and 40-60 mg per day, respectively.  Tablets of Proviron should not be chewed and must always be swallowed with a full glass of water. Overdosing or abuse of this drug can lead to health complications such as oily skin, acne, exacerbation of male pattern baldness, growth of body/facial hair, deepening of the voice, and menstrual irregularities. The use of Mesterolone is not recommended to patients with carcinoma of the prostate or those who are undergoing androgen therapy of any kind, including the use of GP Proviron. In case a dose of this drug has been missed and it is almost time for the next dose, the first dose should be ignored and the next dose should be taken at the designated time. Under no circumstances, two doses of the drug should be taken together for the dose that was missed. Medical advice should be sought without any delay and use of GP Proviron should be stopped immediately if side effects such as pain in liver area, headache, loss of appetite, depression, unexplained weight loss, aggression, symptoms of an enlarged prostate (change in urination), acne or hirsutism are experienced.

Friday, April 3, 2015

Effect of Tamoxifen Citrate in bodybuilding life

When it comes to treating advanced breast cancer patients or reducing the side effects of estrogens while coming off their anabolic steroid cycle, Nolvadex, also known as Tamoxifen citrate. For on cycle gynecomastia prevention and post cycle therapy (PCT) needs Tamoxifen Citrate often fills the role of both for many performance enhancers across the board. For decades Tamoxifen Citrate has been a staple in many cycles in both men and women and for good reason; it works, it works well and is in most cases very well-tolerated.

By its mode of action Tamoxifen Citrate functions of the basis of two hormones, estrogen and testosterone, discouraging one while promoting the other. Belonging to a class of medications known as Selective Estrogen Receptor Modulators (SERM’s) Tamoxifen Citrate is not an anabolic steroid in any shape form or fashion, it does not perform in the traditional anabolic nature, although it can provide a secondary anabolic effect by its method of testosterone stimulation. Since Nolvadex has the ability of inhibiting the growth of tumors that respond to estrogens, it is one of the most popular drugs for treating node-positive breast cancer in women following total mastectomy or segmental mastectomy, axillary dissection, and breast irradiation. The antiestrogen is also recommended for treating metastatic breast cancer in women and men and Nolvadex is an alternative to oophorectomy or ovarian irradiation in premenopausal women with metastatic breast cancer. Medically, it is advised for the treatment of breast cancer that has spread to other parts of the body (metastatic breast cancer) and is also advised to treat breast cancer in certain patients after surgery and radiation therapy and may even be suggested to minimize the chances of breast cancer in high-risk patients.

For its testosterone stimulating properties this will be and is the main reason any anabolic steroid user will supplement with Tamoxifen Citrate and this will occur during the PCT period for men. When we supplement with anabolic steroids our natural testosterone production is suppressed and once the cycle is complete it is imperative that we once again stimulate natural testosterone production. This is very important to our overall health, as a well-functioning endocrine system is more than necessary; however it is also imperative to maintaining the gains made while on a cycle of anabolic steroids. While Tamoxifen Citrate therapy will not return natural testosterone production to its normal state during PCT use it will send you well on your way. A common misconception is that with a good PCT program our natural testosterone levels are normalized by this simple 3-4 week process, unfortunately this simply isn’t true. Assuming no more anabolic steroids are applied it can take several months for normal levels to be obtained even with Tamoxifen Citrate therapy; however, without therapy such normalization can take up to as much as a year or more depending on the individual at hand.

Beyond PCT needs Tamoxifen Citrate is often used as a means of gynecomastia prevention while on a cycle of anabolic steroids. Many anabolic steroids of an androgenic nature, such as testosterone will convert into estrogen after administration. Estrogen is an essential hormone for proper bodily function in-terms of sexual function, immune system and muscle growth, we do need some, however, as these levels increase it can become quite problematic. Many of the most commonly associated side-effects of anabolic steroid use are due to this conversion process brought on by the aromatase enzyme and as levels increase side-effects rear their head. A very common misconception is that Tamoxifen Citrate decreases estrogen in the body in the same fashion as many aromatase inhibitors; this is not true. While it will not reduce estrogen Tamoxifen Citrate will block it from binding to the receptors thereby preventing side-effects such as gynecomastia. Generally 10mg every day of the medication will prove to be useful for this end, however, for many no amount will be enough and only an aromatase inhibitor will prove to be effective.

While Tamoxifen Citrate was not created with performance enhancing in mind it is just that for which it is used most commonly and without question it has proven to be one of the most useful tools in the arsenal of any performance enhancer. Available in both tablet and liquid forms you simply drink there really aren’t too many downsides to this medication, in-fact, most well-planned cycles, be it for on cycle or PCT use will include Tamoxifen Citrate in them at some point and time as it is a highly necessary medication for most any athlete.

One of the biggest advantages of this antiestrogen is that patients whose tumors are estrogen receptor positive are more likely to benefit from it. In addition to that, it can minimize the occurrence of contralateral breast cancer in patients receiving adjuvant therapy for breast cancer. In women with Ductal Carcinoma in Situ (DCIS) after breast surgery and radiation, Nolvadex (Tamoxifen citrate) can minimize the risk of invasive breast cancer. It is worthwhile to note that Tamoxifen citrate is well tolerated in males with breast cancer and safety profile of the drug in males is similar to that noticed in women.

Sportsmen using anabolic steroids and performance enhancing drugs like Dianabol, Anadrol, and Testosterone derivatives often make use of Nolvadex (Tamoxifen citrate) and medical studies in the past have suggested that use of this antiestrogen is associated with dramatic improvements in levels of luteinizing hormone, follicle-stimulating hormone, testosterone, and estrogen control.  Since use of Nolvadex is featured by its mild yet highly effective properties, it is often preferred compared to Arimidex, Femara and Aromasin since it does not prevent aromatization but plays the role of an estrogen antagonist, which is also useful in burning fat. The recommended dose of Nolvadex for patients with Ductal Carcinoma in Situ (DCIS) is 20 mg daily for 5 years while sportsmen on steroids use it in doses of 20-45 mg per day, with or without food.

Nolvadex (Tamoxifen citrate) abuse can lead to side effects, which may be mild or severe, including hypercalcemia, peripheral edema, distaste for food, pruritus vulvae, depression, dizziness, light-headedness, headache, hair thinning and/or partial hair loss, and vaginal dryness. In very rare cases, side effects like erythema multiforme, Stevens-Johnson syndrome, bullous pemphigoid, interstitial pneumonitis and rare reports of hypersensitivity reactions including angioedema may happen.

Women keen to use Tamoxifen citrate should avoid getting pregnant for two months after last stopping its use and others should best use birth control methods that don’t use hormones like diaphragms with spermicide or plain intrauterine devices (IUDs). Moreover, breast-feeding is not recommended while using this drug as it is unknown of Nolvadex passes into breast milk or may cause potential risk to the infant. Nolvadex (Tamoxifen citrate) is not recommended to individuals suffering with high amount of calcium in the blood, severely decreased platelets, decreased white blood cells, cataracts, problems with eyesight, blood clot in lung, stroke, obstruction of a blood vessel by a blood clot, blood clot in a deep vein, pregnancy, or a mother who is producing milk and breastfeeding. A loss of sexual ability or interest may occur in men making use of Nolvadex.